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Preparation and evaluation of mucinated sodium alginate microparticles for oral delivery of insulin.
Eur J Pharm Biopharm. 2008 Nov; 70(3):777-83.EJ

Abstract

Effective oral insulin delivery remains a challenge to the pharmaceutical industry. In this study, insulin-loaded microparticles for oral delivery were prepared with mucin and sodium alginate combined at different ratios using a novel method based on polymer coacervation and diffusion filling. Some physical characteristics of the various insulin-loaded microparticles such as particle size, morphology and compressibility indices were determined. The microparticles were filled into hard gelatin capsules and the in vitro insulin release as well as the blood glucose reduction after oral administration to diabetic rabbits were determined. The microparticles formed were generally multi-particulate, discrete and free flowing. Before insulin loading, microparticles were round and smooth, becoming fluffier, less spherical and larger with rough and pitted surface after insulin loading. The insulin content of the microparticles increased with increase in their sodium alginate content. The various insulin-loaded microparticles prepared with the mucinated sodium alginate when encapsulated exhibited lag time before insulin release. The time taken to reach maximum insulin release from the various formulations varied with the mucin-sodium alginate ratio mix. The mean dissolution time of insulin from the microparticles prepared with sodium alginate, mucin, sodium alginate: mucin ratios of 1:1, 3:1 and 1:3 was 11.21+/-0.75, 3.3+/-0.42, 6.69+/-023, 8.52+/-0.95 and 3.48+/-0.65 (min.), respectively. The percentage blood glucose reduction for the subcutaneously administered insulin was significantly (p<0.001) higher than for the formulations. The blood glucose reduction effect produced by the orally administered insulin-loaded microparticles prepared with three parts of sodium alginate and one part of mucin after 5h was, however, equal to that produced by the subcutaneously administered insulin solution, an indication that it is an effective alternative for the delivery of insulin.

Authors+Show Affiliations

Department of Pharmaceutical Technology and Raw Material Development, National Institute for Pharmaceutical Research and Development, Abuja, Nigeria. philonsky@yahoo.comNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

18644444

Citation

Builders, Philip F., et al. "Preparation and Evaluation of Mucinated Sodium Alginate Microparticles for Oral Delivery of Insulin." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 70, no. 3, 2008, pp. 777-83.
Builders PF, Kunle OO, Okpaku LC, et al. Preparation and evaluation of mucinated sodium alginate microparticles for oral delivery of insulin. Eur J Pharm Biopharm. 2008;70(3):777-83.
Builders, P. F., Kunle, O. O., Okpaku, L. C., Builders, M. I., Attama, A. A., & Adikwu, M. U. (2008). Preparation and evaluation of mucinated sodium alginate microparticles for oral delivery of insulin. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 70(3), 777-83. https://doi.org/10.1016/j.ejpb.2008.06.021
Builders PF, et al. Preparation and Evaluation of Mucinated Sodium Alginate Microparticles for Oral Delivery of Insulin. Eur J Pharm Biopharm. 2008;70(3):777-83. PubMed PMID: 18644444.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Preparation and evaluation of mucinated sodium alginate microparticles for oral delivery of insulin. AU - Builders,Philip F, AU - Kunle,Olobayo O, AU - Okpaku,Larry C, AU - Builders,Modupe I, AU - Attama,Anthony A, AU - Adikwu,Michael U, Y1 - 2008/07/03/ PY - 2007/12/11/received PY - 2008/06/17/revised PY - 2008/06/19/accepted PY - 2008/7/23/pubmed PY - 2009/1/24/medline PY - 2008/7/23/entrez SP - 777 EP - 83 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 70 IS - 3 N2 - Effective oral insulin delivery remains a challenge to the pharmaceutical industry. In this study, insulin-loaded microparticles for oral delivery were prepared with mucin and sodium alginate combined at different ratios using a novel method based on polymer coacervation and diffusion filling. Some physical characteristics of the various insulin-loaded microparticles such as particle size, morphology and compressibility indices were determined. The microparticles were filled into hard gelatin capsules and the in vitro insulin release as well as the blood glucose reduction after oral administration to diabetic rabbits were determined. The microparticles formed were generally multi-particulate, discrete and free flowing. Before insulin loading, microparticles were round and smooth, becoming fluffier, less spherical and larger with rough and pitted surface after insulin loading. The insulin content of the microparticles increased with increase in their sodium alginate content. The various insulin-loaded microparticles prepared with the mucinated sodium alginate when encapsulated exhibited lag time before insulin release. The time taken to reach maximum insulin release from the various formulations varied with the mucin-sodium alginate ratio mix. The mean dissolution time of insulin from the microparticles prepared with sodium alginate, mucin, sodium alginate: mucin ratios of 1:1, 3:1 and 1:3 was 11.21+/-0.75, 3.3+/-0.42, 6.69+/-023, 8.52+/-0.95 and 3.48+/-0.65 (min.), respectively. The percentage blood glucose reduction for the subcutaneously administered insulin was significantly (p<0.001) higher than for the formulations. The blood glucose reduction effect produced by the orally administered insulin-loaded microparticles prepared with three parts of sodium alginate and one part of mucin after 5h was, however, equal to that produced by the subcutaneously administered insulin solution, an indication that it is an effective alternative for the delivery of insulin. SN - 0939-6411 UR - https://www.unboundmedicine.com/medline/citation/18644444/Preparation_and_evaluation_of_mucinated_sodium_alginate_microparticles_for_oral_delivery_of_insulin_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939-6411(08)00235-X DB - PRIME DP - Unbound Medicine ER -